Noninsulin Diabetes Medications Summary Chart Medications marked with an asterisk (*) can cause MED GROUP DESCRIPTOR INSULIN SECRETAGOGUES Sulfonylureas* GLYBURIDE* (Diabeta) (Micronase) MICRONIZED GLYBURIDE* (Glynase Prestabs) 1.25, 2.5, 5 Take to avoid 1.5, 3, 6 1.25 20 0.75 12 GLIPIZIDE* (Glucotrol) 5, 10 30 minutes premeal 2.5 40 GLIPIZIDE EXTENDED * (Glucotrol Xl) 2.5, 5, 10 5 20 GLIMEPIRIDE* (Amaryl) 1, 2, 4 1 time/day 0.5 8 Meglitinides* REPAGLINIDE* (Prandin) D-Phenylalanine Derivative* 0.5, 1, 2, 4 2 4 times/day, 0 30 min premeals Add meal, add dose to total of 4 doses/day 0.5 16 NATEGLINIDE* (Starlix) GLUCOSE SUPPRESSORS 60, 120 1 3 times/day, 0 30 min premeals 180 360 Biguanides METFORMIN (Glucophage) Action: Decreases hepatic glucose and improves glucose transport 500, 850, 1000 2 4 times/day Take to avoid stomach upset 500 2550 Side effects: Gas, diarrhea, lactic acidosis. To decrease lactic acidosis risk, avoid in: Liver disease, alcohol abuse/bingeing If creatinine 1.4 mg/dl in women; 1.5 mg/dl in men IV contrast If creatinine clearance 50 ml/min Recurrent CHF Severe infection, acute MI Hold for IV contrast dye, surgery, or severe vomiting or diarrhea. Repeat creat. in 48 hrs; if OK, restart metformin Note: Take with to decrease gas, diarrhea Copyright 2012 Joslin Diabetes Center. All rights reserved.
METFORMIN SUSTAINED (Glucophage XR) METFORMIN EXTENDED (Fortamet) METFORMIN EXTENDED (Glumetza) METFORMIN ORAL SOLUTION (Riomet) INSULIN SENSITIZERS Thiazolidinediones See above 500, 750 500, 1000 1 time/day 500, 1000 1 time/day 500 mg/5 ml 2 3 times/day 500 2000 500 2500 500 2500 500 2550 ROSIGLITAZONE (Avandia) Note: The FDA has now determined that in addition to describing the cardiovascular risks (such as heart attack or stroke ) of rosiglitazone and rosiglitazone-containing medicines, the drug labels must be revised to state that use of the drug is limited to: Patients already being treated with these medicines Patients whose blood sugar cannot be controlled with other antidiabetic medicines and who, after consulting with their healthcare professional, do not wish to use pioglitazone-containing medicines (Actos, Actoplus Met, Actoplus Met XR, or Duetact) PIOGLITAZONE (Actos) Action (both): Improves glucose transport and decreases hepatic glucose ; may have beneficial effect on endothelium Side effects (both): Weight gain, fluid retention, osteopenia, increase in CHF in those at risk Liver disease check LFTs at baseline, then periodically (both): May cause resumption of ovulation in perimenopausal women Take same time daily May require up to 2 weeks to see an effect 2, 4, 8 15, 30, 45 1 time/day 4 8 15 45 DPP-4 INHIBITORS SITAGLIPTIN PHOSPHATE (Januvia) Action: Slows the inactivation of increased insulin synthesis and decreased glucagon levels in a glucose-dependent manner 25, 50, 100 25 100 SAXAGLIPTIN (Onglyza) LINAGLIPTIN (Tradjenta) Side effects: URI, stuffy nose, sore throat, occasional diarrhea and stomach discomfort; UTI with Onglyza : Decrease dose for renal disease (Januvia and Onglyza). Watch for interactions with drugs that induce CYP450 3A4 (Tradjenta) Watch for interactions with drugs that inhibit CYP450 3A4 (Onglyza) 2.5, 5 5 2
STARCH BLOCKERS Alpha-Glucosidase Inhibitors MIGLITOL (Glyset) Action: Delays absorption and breakdown of carbohydrates from intestines 25, 50, 100 3 times/day With first bite of meal 25 300 ACARBOSE (Precose) Side effects: Gas, diarrhea; elevation of LFTs with acarbose in doses >50 mg tid, and wt < 132 lbs 25, 50, 100 3 times/day With first bite of meal 25 300 : Use glucose to treat when in combination therapy Dose low and increase slowly to decrease flatulence BILE ACID SEQUESTRANTS COLESEVELAM (Welchol) Action: Reduces LDL cholesterol and improves glycemic control Side effects: Constipation, nausea, diarrhea, gas, heartburn, headache; may interact with glyburide, levothyroxine, and contraceptives 625 mg tablet 1.875 g, 3.75 g powder packet 6 tablets (or 3.75 g powder packet) daily or 3 tablets (or 1.875 g powder packet) twice daily with a meal and liquid 1875 3750 DOPAMINE AGONIST BROMOCRIPTINE MESYLATE* (Cycloset) Action: Unknown; lowers glucose without increasing insulin; reduces the risk of MI and stroke 0.8mg 1 time/day with within 2 hrs of waking 1.6 4.8 FIXED COMBINATIONS GLYBURIDE and METFORMIN* (Glucovance) Side effects: Hypotension, orthostatic changes, fainting, drowsiness, may worsen psychotic disorders,, nausea, fatigue, severe dizziness and decreases hepatic glucose 1.25 mg/250 mg 2. GLIPIZIDE and METFORMIN* (Metaglip) ROSIGLITAZONE and METFORMIN (Avandamet ) PIOGLITAZONE and METFORMIN (Actoplus Met) sulfonylureas and biguanides Action: Improves glucose transport and decreases hepatic glucose thiazolidinediones and biguanides 2.5 mg/250 mg 2. 1 mg/500 mg 2 mg/500 mg 4 mg/500 mg 2 mg/1000 mg 4 mg/1000 mg 1 15 mg/850 mg 15 45 mg/ 500 2250 REPAGLINIDE and METFORMIN (Prandimet) and decreases hepatic glucose meglitinides and biguanides See note under thiazolidinediones regarding limitations on use 1 mg/500 mg 2 mg/500 mg 2-3 times/day 15 minutes pre-meal Max dose 10 mg/2500 mg 3
ROSIGLITAZONE and GLIMEPIRIDE* (Avandaryl ) Action: Improves glucose transport, decreases hepatic glucose, and stimulates β-cell insulin 4 mg/1 mg 4 mg/2 mg 4 mg/4 mg 1 time/day with first meal PIOGLITAZONE and GLIMEPRIDE* (Duetact) SITAGLIPTIN and METFORMIN (Janumet) SAXAGLIPTIN and METFORMIN XR (Kombiglyze XR) thiazolidinediones and sulfonylureas Action: Improves insulin action in adipose tissue, liver, and skeletal muscle; may have beneficial effect on vascular cells and β cells; stimulates β-cell insulin pioglitazone and glimepride Action: Slows the inactivation of increased insulin synthesis and decreased glucagon levels in a glucose-dependent manner; decreases hepatic glucose and improves glucose transport sitagliptin and metformin; reduce Kombiglyze to 2.5 mg/1000 mg if also taking strong CYP3A415 inhibitors, such as ketoconazole 15 mg, 30 mg, 45 mg 50 mg sitagliptin/500 ; 50 mg sitagliptin/1000 5 mg /1000 mg 2.5 mg /1000mg 1 time/day before first meal 2 times/ day, taken with 1 time/day with evening meal Start at 15 mg/day Increase every 4 to 8 weeks or more, as needed, to 30 mg/day, and then to 45 mg/day LINAGLIPTIN and METFORMIN (Jentadueto) See note under thiazolidinediones regarding limitations on use linagliptin/500 linagliptin/850 linagliptin/1000 2 times/day 4
Injectables GLP-1 RECEPTOR AGONISTS* EXENATIDE (Byetta) EXENATIDE EXTENDED- (Bydureon) LIRAGLUTIDE (Victoza) Action: Increases the level of enhanced insulin secretion and reduced glucagon secretion in a glucose-dependent manner Side effects: Nausea, anorexia, vomiting (mcg or mg/dose) 5 or 10 mcg/dose 2 mg/dose (single-dose tray) 0.6, 1.2, 1.8 mg/dose 2 times/day 0 60 min premeals (6+ hours apart) (mcg or mg/day or week) 10 20 mcg/day 1 time/week 2 mg/week 1 time/day 1.2 1.8 mg/day (initiate at 0.6 mg/d) AMYLIN MIMETIC* PRAMLINTIDE (Symlin) Action: Exact mechanism unknown; decreases postprandial glucose, suppresses glucagon secretion, slows gastric emptying similar to GLP-1 agonists Side effects: Nausea, anorexia, vomiting Type 2 60 120 mcg Type 1 15 60 mcg containing 250 calories or 30 grams of carbohydrates 180 360 mcg/day 30 180 mcg/day 5